mGluR Activator

β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride activates mGluR3 and inhibits PKC. β-N-methylamino-L-alanine hydrochloride can be used in the research of neurodegenerative diseases and immune diseases.

Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC₅₀ of 45 nM and a K_i of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis indica.

ADX88178 is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC₅₀ of 3.5 nM against hmGluR4. ADX88178 modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease.

Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca²⁺ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.

VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC₅₀s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy.

JNJ-46356479 is a blood-brain barrier-penetrant mGluR2/3 allosteric activator. JNJ-46356479 binds to the mGluR2 PAM site to enhance mGluR2 activity, thereby inhibiting presynaptic glutamate release and modulating adenylate cyclase (Adenylate Cyclase), calcium channel (CRAC Channel) activity, and neuronal excitability. JNJ-46356479 exhibits anticonvulsant activity in psychomotor seizures and corneal kindling, and can be used in the study of schizophrenia and epilepsy.

Fasoracetam (NS105) is an orally active metabotropic glutamate receptor (mGluR) activator. Fasoracetam bidirectionally regulates adenylyl cyclase activity and cAMP levels by activating group I-III mGluRs, upregulating GABAB receptors, and enhancing cholinergic neurotransmission. Fasoracetam can be used in research on attention deficit hyperactivity disorder (ADHD), depression, dementia, Alzheimer's disease, and forebrain ischemia.

ZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC₅₀ of 2.4 nM and K_i of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury.

β-N-methylamino-L-alanine hydrochloride (Standard) (BMAA hydrochloride (Standard)) is the analytical standard of β-N-methylamino-L-alanine hydrochloride (HY-W015546). This product is intended for research and analytical applications. β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride activates mGluR3 and inhibits PKC. β-N-methylamino-L-alanine hydrochloride can be used in the research of neurodegenerative diseases and immune diseases.

Talaglumetad (LY-544344) is an orally active prodrug of Eglumegad (HY-18941) and a metabotropic glutamate receptor 2/3 (mGluR2/3) agonist. Talaglumetad undergoes transmembrane transport via the intestinal peptide transporter hPepT1, and is enzymatically hydrolyzed to produce L-alanine and the parent drug Eglumegad after entering the body. Talaglumetad can be used in research related to metabotropic glutamate receptor 2-associated neurological systems.

VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC₅₀ of 1.6 μM. VU0364289 shows excellent central nervous system penetration. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research.

FO-4-15 is an mGluR1/CaMKIIα activator. FO-4-15 has a protective effect against H₂O₂ in human neuroblastoma (SH-SY5Y) cells. FO-4-15 can improve cognitive impairment in Alzheimer’s disease mice by activating the mGluR1/CaMKIIα pathway, and can reduce Aβ accumulation, hyperphosphorylated Tau, and synaptic damage.

VU0477886 is a metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator with potent activating activity on mGlu4 (EC₅₀ = 95nM, 89% Glu Max), good pharmacokinetic characteristics (brain: plasma Kp = 1.3), and significant therapeutic efficacy in Parkinson's disease models.

ADX88178 TFA is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC₅₀ of 3.5 nM against hmGluR4. ADX88178 TFA modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 TFA reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 TFA can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease.

mGluR1 activator-1 is a stable Vitamin K (HY-B2172) analogue and a mGluR1 activator that can penetrate the blood-brain barrier. mGluR1 activator-1 exhibits strong transcriptional activation via steroid and xenobiotic receptor as well as retinoic acid receptor. mGluR1 activator-1 induces neuronal differentiation in mouse neural progenitor cells. mGluR1 activator-1 can be used for the study of neurodegenerative disease such as Alzheimer’s.

(Rac)-LY-2300559 is a positive allosteric modulator of metabotropic glutamate receptor 2 (mGlu2) and an antagonist of cysteinyl leukotriene 1 (CysLT1) receptor, with both EC₅₀ and IC₅₀ values less than 12.5 μM. (Rac)-LY-2300559 enhances glutamate-induced mGlu2 receptor signaling while exerting antagonistic activity against the CysLT1 receptor. (Rac)-LY-2300559 can be used in migraine-related research.

Nefiracetam (Standard) is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca²⁺ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research.

Fasoracetam (NS 105) Standard is the analytical standard of Fasoracetam (HY-107481). This product is intended for research and analytical applications. Fasoracetam (NS105) is an orally active metabotropic glutamate receptor (mGluR) activator. Fasoracetam bidirectionally regulates adenylyl cyclase activity and cAMP levels by activating group I-III mGluRs, upregulating GABAB receptors, and enhancing cholinergic neurotransmission. Fasoracetam can be used in research on attention deficit hyperactivity disorder (ADHD), depression, dementia, Alzheimer's disease, and forebrain ischemia.